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Assay Detail

CHEMBL968439

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at mouse PPARgamma by chimeric transactivation assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL2459)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
Casimiro-Garcia A, Bigge CF, Davis JA, Padalino T, Pulaski J, Ohren JF, McConnell P, Kane CD, Royer LJ, Stevens KA, Auerbach BJ, Collard WT, McGregor C, Fakhoury SA, Schaum RP, Zhou H.
Bioorg Med Chem (2008) 16 : 4883 -4907
PubMed 18394907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.66 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477095 1 6.99
CHEMBL479002 1 6.82
CHEMBL478725 1 6.57
CHEMBL477323 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477095 EC50 = 102.0 nM 6.99
CHEMBL479002 EC50 = 151.0 nM 6.82
CHEMBL478725 EC50 = 272.0 nM 6.57
CHEMBL477323 EC50 = 536.0 nM 6.27